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1. 发明申请

WO2006095020A1 HETEROCYCLIC-SUBSTITUTED ALKANAMIDES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂有用的杂环取代的烷烃
公开(公告)号：WO2006095020A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060625
申请日：2006-03-10
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
IPC分类号： C07C237/20 , C07D307/14 , C07D321/08 , C07D211/58 , C07D307/52 , C07D307/93 , C07D207/14 , C07D205/04 , C07D319/12 , C07D493/08 , C07D309/04 , C07D311/96 , C07D309/14 , C07D303/36 , C07D311/94
CPC分类号： C07D309/06 , C07C237/20 , C07D207/14 , C07D211/58 , C07D303/36 , C07D307/00 , C07D307/14 , C07D307/20 , C07D307/52 , C07D307/93 , C07D309/08 , C07D309/10 , C07D311/00 , C07D311/94 , C07D311/96 , C07D313/14 , C07D319/12 , C07D319/14 , C07D321/08 , C07D493/08
摘要： Compounds of the general formula (I) in which the meanings of the substituents R 1 and R 2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：其中取代基R 1和R 2的含义如权利要求1所述的通式（I）的化合物具有肾素抑制性质并且可以使用作为药物

2. 发明申请

WO2007031558A1 5-AMINO-4-HYDROXY-7- (IMIDAZO [1,2-A] PYRIDIN-6- YLMETHYL)-8-METHYL-NONAMIDE DERIVATIVES AND RELATED COMPOUNDS AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译： 5-氨基-4-羟基-7-（咪唑并[1,2-A]吡啶-6-基]甲基）-8-甲基壬酰胺衍生物及相关化合物作为治疗高血压的RININ抑制剂
公开(公告)号：WO2007031558A1
公开(公告)日：2007-03-22
申请号：PCT/EP2006/066369
申请日：2006-09-14
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , STOJANOVIC, Aleksandar , MARTI, Christiane , BEHNKE, Dirk , JELAKOVIC, Stjepan
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , STOJANOVIC, Aleksandar , MARTI, Christiane , BEHNKE, Dirk , JELAKOVIC, Stjepan
IPC分类号： C07D471/04 , C07D405/12 , A61K31/443 , A61K31/4433 , A61K31/437 , A61P9/12 , A61P9/10
CPC分类号： C07D405/12 , C07D471/04
摘要： Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is -CH 2 -; R 1 is a mono- to tetrasubstituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R 2 is C 1-6 alkyl or C 3-6 cycloalkyl; R 3 is independently of one another H, C 1-6 alkyl, C 1-6 alkoxycarbonyl or C 1-6 alkanoyl; R 4 is C 2-6 alkenyl, C 1-6 alkyl, unsubstituted or substituted aryl- C 1-6 alkyl or C 3-8 cycloalkyl; R 5 is -L m -R 6 ; L is C 1-6 alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n = 0, 1 or 2; m = 0 or 1; R 6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C 1-6 alkyl, C 1-6 alkoxy, cyano, halogen, C 1-6 alkoxy- C 1-6 alkyl, hydroxy-C 1-6 alkyl or dialkylamino, or if m = 0: is also saturated C 3-8 heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C 1-6 alkyl, C 1-6 alkoxy, cyano, halogen, C 1-6 alkoxy- C 1-6 alkyl, hydroxy- C 1-6 alkyl or dialkylamino, or if m = 1: is also saturated C 3-8 heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C 1-6 alkyl, C 1-6 alkoxy, cyano, halogen, C 1-6- alkoxy-C 1-6 alkyl, hydroxy-C 1-6 alkyl or dialkylamino; have renin- inhibiting properties and can be used as medicines for the treatment of hypertension.
摘要翻译：通式（I）的化合物或其盐或其中一个或多个原子被其稳定的非放射性活性同位素替代的化合物，特别是其药学上可接受的盐; 其中X是-CH 2 - ; R 1是具有1至4个氮原子的单 - 四取代，单或双环不饱和杂环基，R 2是C 1-6 - 烷基或C 3-6环烷基; R 3彼此独立地为H，C 1-6烷基，C 1-6烷氧基羰基或C 1-6烷基， / SUB>烷酰基; R 4是C 2-6链烯基，C 1-6烷基，未取代或取代的芳基-C 1-6烷基，烷基或C 3-8环烷基; R 5是-L m -R 6; L是任选被1-4个卤素取代的C 1-6亚烷基或连接基：式（II）n = 0,1或2; m = 0或1; R 6是由选自双环[xyz]烷基，螺[op]烷基，单或生双环[xyz]烷基或单或者生物密封[op]烷基的2个环状体组成的基团，全部其可以被1-3个选自C 1-6烷基，C 1-6 - 烷氧基，氰基，卤素，C 1-6 - 烷基的取代基取代，烷基，C 1-6烷基或二烷基氨基，或者如果m = 0，也是饱和的C 3 -C 6烷基， 8个杂环基，其包含1-2个氧原子，被1-3个选自C 1-6 - 烷基，C 1-6 - 烷氧基，氰基，卤素，C 1-6烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基，或者如果m = 1 ：也包括1-2个氧原子的饱和C 3-8杂环基，任选地被1-3个选自C 1-6烷基的取代基取代，C 1 -C 6烷基， 1-6烷氧基，氰基，卤素，C 1-6 - 烷氧基-C 1-6烷基，羟基-C 1-6烷基，烷基或二烷基氨基; 具有肾素抑制性质，可用作治疗高血压的药物。

3. 发明申请

WO2006103277A3 2 , 4 , 5-SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS 审中-公开
公开(公告)号：WO2006103277A3
公开(公告)日：2006-10-05
申请号：PCT/EP2006/061197
申请日：2006-03-30
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane , STUTZ, Stefan , JELAKOVIC, Stjepan , HOLLINGER, Frank , KONTEATIS, Zenon D. , LUDINGTON, Jennifer L. , QUIRMBACH, Michael , STOJANOVIC, Aleksandar , BEHNKE, Dirk
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane , STUTZ, Stefan , JELAKOVIC, Stjepan , HOLLINGER, Frank , KONTEATIS, Zenon D. , LUDINGTON, Jennifer L. , QUIRMBACH, Michael , STOJANOVIC, Aleksandar , BEHNKE, Dirk
IPC分类号： C07D413/12 , C07D413/14 , A61K31/445
摘要： Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.

4. 发明申请

WO2007031557A2 ALCANOIC ACID AMIDES SUBSTITUTED BY SATURATED O-HETEROCYCLES 审中-公开
标题翻译：饱和脂肪酸取代的氨基酸
公开(公告)号：WO2007031557A2
公开(公告)日：2007-03-22
申请号：PCT/EP2006/066368
申请日：2006-09-14
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
CPC分类号： A61K31/335
摘要： Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：取代基R 1〜R 6的含义如权利要求1所示的通式（式I）的化合物具有肾素抑制性质，可用作药物。

5. 发明申请

WO2007082907A1 SUBSTITUTED 4-PHENYLPIPERIDINES 审中-公开
标题翻译：取代的4-苯基哌啶
公开(公告)号：WO2007082907A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050481
申请日：2007-01-18
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JOTTERAND, Nathalie , STOJANOVIC, Aleksandar , STUTZ, Stefan , JELAKOVIC, Stjepan , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JOTTERAND, Nathalie , STOJANOVIC, Aleksandar , STUTZ, Stefan , JELAKOVIC, Stjepan , QUIRMBACH, Michael
IPC分类号： C07D413/12 , C07D413/14 , A61P9/12 , A61K31/538
CPC分类号： C07D401/12 , C07D413/12 , C07D413/14
摘要： The application relates to substituted 4-phenylpiperidines of the general formula and their salts, preferably their pharmaceutically acceptable salts, in which R 2 , R 3 , W and X have the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式的取代的4-苯基哌啶及其盐，优选其药学上可接受的盐，其中R 2，R 3，W和X具有如下含义：在说明书中解释，其制备方法和这些化合物作为药物的使用，特别是作为肾素抑制剂。

6. 发明申请

WO2007116101A1 IMIDAZO COMPOUNDS 审中-公开
标题翻译：咪唑化合物
公开(公告)号：WO2007116101A1
公开(公告)日：2007-10-18
申请号：PCT/EP2007/053587
申请日：2007-04-12
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , STUTZ, Stefan
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , STUTZ, Stefan
IPC分类号： C07D498/04
CPC分类号： C07D513/04 , C07D498/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R 1 , R 2 , Q, m and n have the meanings explained in detail in the description and * designates an asymmetric carbon atom, a process for their preparation and the use of these compounds as medicaments, in particular as aromatase inhibitors.
摘要翻译：本申请涉及通式（I）的新型杂环化合物及其盐，优选其药学上可接受的盐，其中R 1，R 2，R 2，Q， m和n具有在说明书中详细解释的含义，*表示不对称碳原子，其制备方法和这些化合物作为药物的用途，特别是芳香酶抑制剂。

7. 发明申请

WO2007116099A1 IMIDAZO COMPOUNDS 审中-公开
标题翻译：咪唑化合物
公开(公告)号：WO2007116099A1
公开(公告)日：2007-10-18
申请号：PCT/EP2007/053585
申请日：2007-04-12
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , STUTZ, Stefan
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , STUTZ, Stefan
IPC分类号： C07D498/04 , C07D513/04 , A61K31/4188 , A61P5/40
CPC分类号： C07D513/04 , C07D498/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R 1 , R 2 , Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译：本申请涉及通式（I）的新型杂环化合物和其盐，优选其药学上可接受的盐，其中R 1，R 2，R 2，Q，m 和n具有在说明书中详细解释的含义，其制备方法和这些化合物作为药物，特别是醛固酮合酶抑制剂的用途。

8. 发明申请

WO2007116098A1 SPIRO-IMIDAZO COMPOUNDS 审中-公开
标题翻译： SPIRO-IMIDAZO化合物
公开(公告)号：WO2007116098A1
公开(公告)日：2007-10-18
申请号：PCT/EP2007/053584
申请日：2007-04-12
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , BENNACER, Bibia , STUTZ, Stefan
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JELAKOVIC, Stjepan , BENNACER, Bibia , STUTZ, Stefan
IPC分类号： C07D491/04 , C07D513/04 , A61K31/5383 , A61K31/542 , A61P5/00
CPC分类号： C07D498/04 , C07D513/04
摘要： Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R 1 , R 1' , Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译：通式（I）的新型杂环化合物及其盐，优选其药学上可接受的盐，其中R 1，R 1，R 1，Q 1，m和n 具有在描述中详细解释的含义，其制备方法和这些化合物作为药物的用途，特别是醛固酮合酶抑制剂。

9. 发明申请

WO2005090304A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2005090304A1
公开(公告)日：2005-09-29
申请号：PCT/EP2005/051241
申请日：2005-03-17
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , QUIRMBACH, Michael , BEHNKE, Dirk , MARTI, Christiane
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , QUIRMBACH, Michael , BEHNKE, Dirk , MARTI, Christiane
IPC分类号： C07D209/12
CPC分类号： C07D209/12 , C07D401/06
摘要： The invention relates to novel amino alcohols of the general formula (I) where X, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
摘要翻译：本发明涉及通式（I）的新型氨基醇，其中X，R 1，R 2，R 3，R 4，R 5和R 6各自如上所定义在描述中详细描述了它们的制备方法和这些化合物作为药物的用途，特别是作为肾素抑制剂。

10. 发明申请

WO2008040764A1 SUBSTITUTED 4-PHENYL PIPERIDINES FOR USE AS RENIN INHIBITORS 审中-公开
标题翻译：用作RENIN抑制剂的取代的4-苯基哌啶
公开(公告)号：WO2008040764A1
公开(公告)日：2008-04-10
申请号：PCT/EP2007/060510
申请日：2007-10-03
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , BEHNKE, Dirk , JOTTERAND, Nathalie , JELAKOVIC, Stjepan
发明人： HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , BEHNKE, Dirk , JOTTERAND, Nathalie , JELAKOVIC, Stjepan
IPC分类号： C07D413/12 , A61K31/445 , A61P9/12
CPC分类号： C07D413/12
摘要： Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R 1 is straight-chain C 1-8 -alkanoyloxy, straight-chain C 1-8 -alkoxy, straight-chain C 1-8 - alkoxy-straight-chain-C 1-8 -alkoxy, straight-chain C 1-8 -alkoxycarbonylamino, straight- chain C 0-8 -alkylcarbonylamino, optionally N-mono- or N,N-di-C 1-8 -alkylated amino or hydroxy or straight-chain omega-hydroxy-C 1-8 -alkyl.
摘要翻译：通式（I）的化合物及其盐，优选其药学上可接受的盐; 其中R 1是直链C 1-8 - 烷酰氧基，直链C 1-8 - 烷氧基，直链C 1-8烷基 - 烷氧基 - 直链-C 1-8烷氧基，直链C 1-8烷氧基羰基氨基，直链C 1-8烷基，链C 0-8烷基羰基氨基，任选的N-单或N，N-二-C 1-8 - 烷基化氨基或羟基或直链ω-羟基 -C _{1-8 - 烷基。}

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